A BB3 receptor antagonist; inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM); selective for BB3 over GRPR and NMBR (IC50s = 16 and >100 μM

ML-18 – 5 mg

Brand:
Cayman
CAS:
1422269-30-4
Storage:
-20
UN-No:
- /

ML-18 is a non-peptide bombesin receptor subtype 3 (BB3) antagonist that inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM).{47246} It is selective for BB3 over the gastrin releasing peptide receptor (GRPR) and the neuromedin B receptor (NMBR) with IC50 values of 16 and >100 μM, respectively, in a radioligand binding assay. ML-18 (16 μM) reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells. It also inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells.  

 

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SKU: 27319 - 5 mg Category:

Description

A BB3 receptor antagonist; inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM); selective for BB3 over GRPR and NMBR (IC50s = 16 and >100 μM, respectively, in a radioligand binding assay); reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells at 16 μM; inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells

Formal name: (αS)-N-[[1-(4-methoxyphenyl)cyclohexyl]methyl]-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-1H-indole-3-propanamide

Synonyms: 

Molecular weight: 569.7

CAS: 1422269-30-4

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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